# US 2019/0167584 A1 · Block copolymers and self-assembling nanoparticles formed therefrom

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- Number: US 2019/0167584 A1
- Document ID: US20190167584A1
- Status: Published application
- Kind: A1
- Application number: 15/832,157
- Filed: 2017-12-05
- Published: 2019-06-06
- Earliest claimed: 2017-12-05
- Assignees: International Business Machines Corporation
- Applicants: International Business Machines Corporation
- Inventors: Dylan Boday; Willy Chin; Mareva B. Fevre; Jeannette Garcia; James L. Hedrick; Eunice Leong; Nathaniel H. Park; Rudy J. Wojtecki; Yi Yan Yang
- Web page: https://patentgrep.com/patent/US20190167584A1

## CPC

- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/6907: {the form being a microemulsion, nanoemulsion or micelle}
- C08G 64/0241: {containing nitrogen}
- C08G 64/025: {containing sulfur}
- C08G 64/183: {containing polyether sequences}
- C08G 81/00: Macromolecular compounds obtained by interreacting polymers in the absence of monomers, e.g. block polymers (involving only carbon-to-carbon unsaturated bond reactions C08F299/00 {; polyester-amides C08G69/44; polyester-imides C08G73/16; polyamides-imides C08G73/14; block- or graft polymers containing polysiloxane sequences C08G77/42})
- C08G 83/008: {Supramolecular polymers}
- A61K 31/12: Ketones
- A61K 31/351: not condensed with another ring
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS

## Abstract

The subject matter of this invention relates to block copolymers (BCPs) and, more particularly, to block copolymers capable of self-assembly into nanoparticles for the delivery of hydrophobic cargos. The BCPs include a hydrophobic block that contains a thioether functional group that is susceptible to oxidation, transforming the solubility of the block from hydrophobic to hydrophilic, thereby releasing the hydrophobic cargo of the nanoparticle.

## Claims

### Claim 1

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer having the structure of formula I:
wherein m is 114 and x is 5.

### Claim at position 2

2-4. (canceled)

### Claim 5 (depends on 1)

The block copolymer of claim 1, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 6

(canceled)

### Claim 7

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer of having the structure of formula I:
wherein m is 228 and x is 10.

### Claim 8

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer having the structure of formula II:
wherein n is 114 and y is 10.

### Claim 9

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer having the structure of formula II:
wherein n is 228 and y is 10.

### Claim 10

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer having the structure of formula III:
wherein p is 114 and z is 5.

### Claim 11

A block copolymer comprising:
a hydrophilic block; and
a hydrophobic block containing at least one thioether functional group, the block copolymer having the structure of formula III:
wherein p is 228 and z is 5.

### Claim at position 10

12-25. (canceled)

### Claim 26 (depends on 5)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 5.

### Claim 27 (depends on 7)

The block copolymer of claim 7, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 28 (depends on 27)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 27.

### Claim 29 (depends on 8)

The block copolymer of claim 8, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 30 (depends on 29)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 29.

### Claim 31 (depends on 9)

The block copolymer of claim 9, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 32 (depends on 31)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 31.

### Claim 33 (depends on 10)

The block copolymer of claim 10, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 34 (depends on 33)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 33.

### Claim 35 (depends on 11)

The block copolymer of claim 11, capable of self-assembly into a nanoparticle in which the hydrophobic block forms a core of the nanoparticle and the hydrophilic block forms a shell of the nanoparticle.

### Claim 36 (depends on 35)

A micellar particle comprising:
a hydrophilic shell; and
a hydrophobic core within the hydrophilic shell,
the hydrophilic shell and the hydrophobic core formed from the nanoparticle of claim 35.